EP0711541A1 - Verwendung von Glukose-Blockern zur Hemmung des Haarwachstums - Google Patents
Verwendung von Glukose-Blockern zur Hemmung des Haarwachstums Download PDFInfo
- Publication number
- EP0711541A1 EP0711541A1 EP94308335A EP94308335A EP0711541A1 EP 0711541 A1 EP0711541 A1 EP 0711541A1 EP 94308335 A EP94308335 A EP 94308335A EP 94308335 A EP94308335 A EP 94308335A EP 0711541 A1 EP0711541 A1 EP 0711541A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- glucose
- hair growth
- phloretin
- compound
- cells
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
- A61Q7/02—Preparations for inhibiting or slowing hair growth
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/347—Phenols
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/35—Ketones, e.g. benzophenone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/36—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
Definitions
- the present invention is directed to a method and a composition for inhibiting hair growth. More particularly, it is directed toward a method employing a glucose blocking compound, e.g. phloretin which is topically administered to areas of unwanted hair growth.
- a glucose blocking compound e.g. phloretin which is topically administered to areas of unwanted hair growth.
- Resting mammalian cells are supplied glucose and oxygen by the circulation of blood.
- the cells utilize the oxygen to convert absorbed glucose into carbon dioxide and water by oxidation.
- This oxidation process yields energy which is used to synthesize adenosine triphosphate (ATP) which is a high energy compound.
- ATP adenosine triphosphate
- Energy contained in the ATP is rapidly released by the liberation of two phosphate groups and becomes available for carrying out biochemical reactions required by cell functions.
- Chemical reactions requiring a thermodynamic expenditure of energy also use the degradation of ATP as a source of energy.
- Rapidly growing cells require energy not only for normal cell functions but also for the synthesis of cellular mass. Such cells utilize glucose as a building block for the formation of new protein and nucleic acids. Rapidly dividing cells utilize aerobic glycolysis, converting glucose to lactic acid instead of carbon dioxide and water. Growing fetal cells and lymphocytes which are stimulated by mitogens have been studied and found to utilize this process. Roos D, Loos JA, "Changes in the Carbohydrate Metabolism of Mitigenically Stimulated Human Peripheral Lymphocytes.” Experimental Cell Research (1973) 77:127-135.
- Circulation of blood to hair follicle cells provides a constant source of glucose. Blood contains close to 100 mg. of glucose/dl and even higher levels after meals. Because the circulation of blood to the hair follicles is excellent, it is not possible to prevent glucose from reaching the hair follicle cells.
- Glucose is water soluble and impermeable to the cell wall. It can only be transported across the cell wall at specific small islands of hydrated protein on the cell surface known as receptor sites.
- the receptor sites on the cell's surface contain specific receptor proteins and utilize enzyme systems to effect the transfer of glucose into the cell by the process of facilitated diffusion. Thus, if the receptor sites are disabled, glucose cannot be adsorbed by the cell despite the constant supply to the cell surface.
- non-metabolizable sugars such as 2-methoxy glucose can block the transfer of glucose.
- their use poisons the enzyme systems.
- glucose blocking compounds that bond to receptor sites may be used to prevent metabolization of glucose.
- Glucose blocking compounds are known, with the earliest having been isolated at the end of the 19th century. The majority of these substances are phenolic compounds of varying complexity some of which are easily synthesized in the laboratory. Le Fevre, P. "Sugar Transport in the Red Blood Cell: Structure-Activity Relationships in Substances and Antagonists.” Pharm. Rev. (1961) 13:39-70.
- Phloridzin is a phenolic compound which functions as a glucoside, blocking receptor sites on cell walls. Phloridzin is a natural plant hormone present in apple root bark, Merck Index 10:7211, 1983, and in the seeds of immature apples. Nature, 158:663, 1946. Intravenous injection of phloridzin causes glucosuria in animals and humans because it blocks absorption of glucose by renal tubular cells, thereby preventing absorption of glucose from the glomerular filtrate. Diedrich, D.F. "The Comparative Effects of Some Phloridzin Analogs on the Renal Absorption of Glucose.” Biochem. Biophys. Acta.
- Phloridzin is known to be very effective in blocking glucose transfer into the renal tubular cells and the cells of the intestinal mucosa where the glucose transport is intimately related to sodium transport. Such glucose transport is known to be sodium dependent. Phloretin, the aglucone of phloridzin, on the other hand has a diminished effect on this type of glucose transfer and parenteral administration may fail to cause glucosuria in animals and man. By contrast, phloretin is much more active on non-sodium dependent transfer of glucose, since non-sodium dependent glucose transport is the normal transfer mechanism of most cells other than those of the renal tubule and intestinal mucosa. This type of transfer has been extensively studied in the red blood cell where precise measurements can be made. Le Fevre, supra. Our studies have shown that glucose transport into the follicular cells which form hair is identical to that found in red blood cells. For this reason, phloretin is much more effective than phloridzin.
- a topically applied composition e.g. a solution
- the present invention provides a composition for inhibiting hair growth in mammals which contains as the active ingredient a compound which blocks glucose transfer across the membranes of the cells of hair follicles.
- the compound is used in a method of inhibiting hair growth in mammals including topically applying the compound e.g. as a solution to any area of unwanted hair on a daily basis.
- a preferred embodiment of the invention uses phloretin as a glucose blocking compound.
- Other embodiments of the invention include steviol, cytochlasin B, 3,3'diallylstilbesterol and 3,3'-di(2-chlorallyl) stilbesterol.
- the blocking compounds are suspended in solutions of suitable solvents which may include propylene glycol and ethyl alcohol.
- the invention also includes a method of inhibiting hair growth on the skin of a mammal by administering topically to the skin a preparation containing a glucose blocking compound.
- Phloretin is a preferred glucose blocking compound. Phloretin is not soluble in aqueous solution, but is soluble in some solvents including propylene glycol, ethyl alcohol, dimethlsufoxide (DMSO) and other solvents. Phloretin prevents the entrance of glucose into cells by blocking the glucose transfer sites on the cell membrane. Phloretin is a complex diphenolic compound, which is the aglucon of phloridzin.
- Phloretin is dissolved in a solution containing 20% propylene glycol and 80% ethyl alcohol to yield a solution having a final concentration of 5-7.5% phloretin.
- the resulting solution is applied topically to any area of unwanted hair growth on a daily basis.
- cytochlasin B which is an effective glucose blocking compound that firmly attaches itself to the glucose receptor protein of a single receptor.
- the uptake of radioactive cytochlasin B is used to determine the number of receptor sites present on a cells surface. Because cytochalasin B is less soluble in propylene glycol and ethyl alcohol some DMSO is added to these solvents.
- Still other embodiments of the present invention include effective glucose blocking compounds such as steviol, 3,3'diallylstilbesterol, and 3,3'-di(2-chlorallyl) stilbesterol.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP94308335A EP0711541A1 (de) | 1994-11-11 | 1994-11-11 | Verwendung von Glukose-Blockern zur Hemmung des Haarwachstums |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP94308335A EP0711541A1 (de) | 1994-11-11 | 1994-11-11 | Verwendung von Glukose-Blockern zur Hemmung des Haarwachstums |
Publications (1)
Publication Number | Publication Date |
---|---|
EP0711541A1 true EP0711541A1 (de) | 1996-05-15 |
Family
ID=8217905
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP94308335A Withdrawn EP0711541A1 (de) | 1994-11-11 | 1994-11-11 | Verwendung von Glukose-Blockern zur Hemmung des Haarwachstums |
Country Status (1)
Country | Link |
---|---|
EP (1) | EP0711541A1 (de) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997019673A2 (en) * | 1995-11-30 | 1997-06-05 | Handelman, Joseph, H. | Reduction of hair growth |
US7722901B2 (en) | 2004-01-16 | 2010-05-25 | Cognis Ip Management Gmbh | Uses for the extract of a plant of the family Asclepiadaceae |
WO2012010624A2 (en) | 2010-07-23 | 2012-01-26 | Dsm Ip Assets B.V. | Topical use of steviol or derivatives in hair care |
JP2012092138A (ja) * | 2011-12-27 | 2012-05-17 | Maruzen Pharmaceut Co Ltd | 皮膚化粧料及び頭髪化粧料 |
WO2016201214A1 (en) * | 2015-06-12 | 2016-12-15 | Stc. Unm | Human glut5 specific inhibitors and methods of treatment |
Citations (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4219569A (en) * | 1978-10-10 | 1980-08-26 | The Upjohn Company | Process for treating inflammation |
EP0291151A1 (de) * | 1984-08-13 | 1988-11-17 | Harry H. Leveen | Zusammensetzungen mit Derivaten von Phlorizin zur Behandlung von Krebs |
EP0383467A2 (de) * | 1989-02-06 | 1990-08-22 | Andries Johannes Cornelus Strydom | Arzneimittel zur Haarausfall- oder/und Schuppen-Bekämpfung |
JPH04124122A (ja) * | 1990-09-14 | 1992-04-24 | Shiseido Co Ltd | 白髪防止黒化剤 |
EP0490581A1 (de) * | 1990-12-07 | 1992-06-17 | Unilever Plc | Kosmetisches Mittel |
JPH04235112A (ja) * | 1991-01-11 | 1992-08-24 | T Ee C Gijutsu Kagaku Kenkyusho:Kk | チロシナーゼ阻害剤 |
EP0532219A2 (de) * | 1991-09-04 | 1993-03-17 | Unilever Plc | Kosmetisches Mittel |
EP0565785A1 (de) * | 1992-04-07 | 1993-10-20 | Harry H. Leveen | Verwendung von Glukosetransporthemmern zur Behandlung von Akné |
FR2704751A1 (fr) * | 1993-05-07 | 1994-11-10 | Oreal | Composition à base de fructose, de glucose et de protéines globulaires de céréale ou leurs hydrolysats, pour diminuer la chute des cheveux et/ou favoriser la repousse des cheveux. |
-
1994
- 1994-11-11 EP EP94308335A patent/EP0711541A1/de not_active Withdrawn
Patent Citations (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4219569A (en) * | 1978-10-10 | 1980-08-26 | The Upjohn Company | Process for treating inflammation |
EP0291151A1 (de) * | 1984-08-13 | 1988-11-17 | Harry H. Leveen | Zusammensetzungen mit Derivaten von Phlorizin zur Behandlung von Krebs |
EP0383467A2 (de) * | 1989-02-06 | 1990-08-22 | Andries Johannes Cornelus Strydom | Arzneimittel zur Haarausfall- oder/und Schuppen-Bekämpfung |
JPH04124122A (ja) * | 1990-09-14 | 1992-04-24 | Shiseido Co Ltd | 白髪防止黒化剤 |
EP0490581A1 (de) * | 1990-12-07 | 1992-06-17 | Unilever Plc | Kosmetisches Mittel |
JPH04235112A (ja) * | 1991-01-11 | 1992-08-24 | T Ee C Gijutsu Kagaku Kenkyusho:Kk | チロシナーゼ阻害剤 |
EP0532219A2 (de) * | 1991-09-04 | 1993-03-17 | Unilever Plc | Kosmetisches Mittel |
EP0565785A1 (de) * | 1992-04-07 | 1993-10-20 | Harry H. Leveen | Verwendung von Glukosetransporthemmern zur Behandlung von Akné |
FR2704751A1 (fr) * | 1993-05-07 | 1994-11-10 | Oreal | Composition à base de fructose, de glucose et de protéines globulaires de céréale ou leurs hydrolysats, pour diminuer la chute des cheveux et/ou favoriser la repousse des cheveux. |
Non-Patent Citations (5)
Title |
---|
D.I. WILKINSON: "Effects of nordihydroguayaretic acid, phloretin and phloridzin on the activity of adenylate cyclase, lipoxygenase and hexose transport, and growth of cultured keratinocytes.", INT. J. DERMATOL., vol. 26, no. 10, pages 660 - 666 * |
DATABASE WPI Derwent World Patents Index; AN 92-189207 [23] * |
M.P. PHILPOTT: "Metabolic studies on isolated hair follicles: Hair follicles engage in aerobic glycolysis and do not demonstrate the glucose fatty acid cycle.", J. INVEST. DERMATOL., vol. 96, no. 6, pages 875 - 879, XP008063099, DOI: doi:10.1111/1523-1747.ep12475232 * |
PATENT ABSTRACTS OF JAPAN vol. 16, no. 584 (C - 1013) * |
STN INTERNATIONAL, KARLSRUHE. FILE CHEMICAL ABSTRACTS. AN=117:219724. * |
Cited By (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997019673A2 (en) * | 1995-11-30 | 1997-06-05 | Handelman, Joseph, H. | Reduction of hair growth |
US5652273A (en) * | 1995-11-30 | 1997-07-29 | Henry; James | Reduction of hair growth |
WO1997019673A3 (en) * | 1995-11-30 | 1997-10-02 | Handelman Joseph H | Reduction of hair growth |
US5824665A (en) * | 1995-11-30 | 1998-10-20 | Henry; James | Reduction of hair growth |
US6218435B1 (en) | 1995-11-30 | 2001-04-17 | James Henry | Reduction of hair growth |
US7722901B2 (en) | 2004-01-16 | 2010-05-25 | Cognis Ip Management Gmbh | Uses for the extract of a plant of the family Asclepiadaceae |
WO2012010624A2 (en) | 2010-07-23 | 2012-01-26 | Dsm Ip Assets B.V. | Topical use of steviol or derivatives in hair care |
WO2012010624A3 (en) * | 2010-07-23 | 2012-09-27 | Dsm Ip Assets B.V. | Topical use of steviol or derivatives in hair care |
JP2012092138A (ja) * | 2011-12-27 | 2012-05-17 | Maruzen Pharmaceut Co Ltd | 皮膚化粧料及び頭髪化粧料 |
WO2016201214A1 (en) * | 2015-06-12 | 2016-12-15 | Stc. Unm | Human glut5 specific inhibitors and methods of treatment |
US10822325B2 (en) | 2015-06-12 | 2020-11-03 | Unm Rainforest Innovations | Human GLUT5 specific inhibitors and methods of treatment |
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PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
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17P | Request for examination filed |
Effective date: 19961115 |
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17Q | First examination report despatched |
Effective date: 19990414 |
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STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION IS DEEMED TO BE WITHDRAWN |
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18D | Application deemed to be withdrawn |
Effective date: 19990601 |